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br LO and the secretase complex Supporting this concept duri
2023-08-01

5LO and the γ-secretase complex Supporting this concept, during a recent trial testing the γ-secretase inhibitor semagacestat (LY 450139), AD patients actually experienced a functional decline compared to patients who took a placebo in addition to several other significant adverse effects (Doody
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br COX and LOX in post mortem
2023-08-01

COX and 5-LOX in post-mortem AD brain Minghetti (2004) reviewed the findings on COX-2 mRNA levels in AD brains, pointing out that the available evidence demonstrated either decreased or increased levels, possibly because of the short half-life of COX-2 transcripts or individual variability. Histo
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However for a molecular target to be
2023-08-01

However, for a molecular target to be useful in AD, it must rescue behavioral as well as biochemical insults. In humans, AD memory impairments typically declare themselves initially as disruption of episodic memory and consolidation of new memories, eventually progressing to global cognitive decline
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br Conflict of interest br Acknowledgments
2023-08-01

Conflict of interest Acknowledgments Introduction Inflammation is a protective response of the microcirculation to harmful stimuli. Yet, excessive inflammation is potentially harmful and a characteristic of many chronic diseases [1]. 5-Lipoxygenase (5-LO, EC1.13.11.34) contributes to the in
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Having established the structural requirements for
2023-08-01

Having established the structural requirements for potency in both the biochemical and biomarker (CRA) assays, we evaluated key compounds in the metabolic stability assay. Disappointingly, we found that all compounds had high intrinsic clearances in mouse microsomes. To ascertain whether the in vitr
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br Methods br Results br Discussion Autotaxin has been
2023-08-01

Methods Results Discussion Autotaxin has been shown to have effects on major cell types implicated in OA, notably chondrocytes, osteoblasts, osteoclasts, and synoviocytes, through its enzymatic product LPA [20]. However, a paucity of research exists on the involvement of autotaxin in OA. Fi
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br Introduction Stroke is a devastating condition that cause
2023-08-01

Introduction Stroke is a devastating condition that causes cognitive and motor dysfunction, neurodegenerative diseases and even acute death, and is a leading cause of mortality and morbidity worldwide (Chen et al., 2014a, Wang et al., 2016). Thus, exploration or identification of novel therapeuti
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The link between HPV infection and neoplasia has
2023-08-01

The link between HPV infection and neoplasia has been well established. HPV encodes two oncogenes (E6 and E7) that drive 98 2 progression by controlling the functions of tumor suppressor proteins p53 and Rb [7]. HPV is associated with more than 99% of cervical CESC cases [8]. CESC remains a major p
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In this study significant reduction in the HCO content in
2023-08-01

In this study, significant reduction in the HCO3− content in sham-operated and testosterone-treated rats following bafilomycin A1 administration suggested that V-ATPase could be involved in mediating the decrease in vas deferens fluid HCO3− content, most probably due to the increase in H+ secretion
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The compounds containing beryllium act
2023-08-01

The compounds containing beryllium act as strong Lewis acids because of electron deficiency of the Be DBIBB []. Interactions of X-Be-Y compounds with different Lewis bases have been studied by Yanez and co-workers [], extensively. Recently, they proposed a class of extremely strong bidentate Be-bas
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In this review we will present the
2023-08-01

In this review, we will present the traditional and actual strategies to study orphan receptors and identify their ligands. An extensive description of the orphan GPCR field has been published in 2013 by Davenport et al. [22]. Therefore, we will focus on the deorphanizations that were reported since
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Based on its kinetic parameters and quaternary structure R p
2023-08-01

Based on its kinetic parameters and quaternary structure, R. pycnus arginase is a typical ureotelic L-arginase [2]. The Km value of the enzyme was lower than other arginases from other organisms (Table 2), including S. cerevisiae (15.7mM), B. anthracis (10mM), B. caldovelox (3.4mM), human liver (2.3
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APJ receptors have a amino acid sequence with a
2023-08-01

APJ receptors have a 380 amino IL-4, murine recombinant australia sequence with a characteristic G-protein structure, including seven transmembrane domains and post-translation modification sites for phosphorylation, palmitoylation and glycosylation along with association sites for β-arrestin (O'Do
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In recent years the higher lipophilicity thus better perform
2023-08-01

In recent years, the ‘higher lipophilicity’-thus-‘better performance’ tenet, derived from the polar paradox theory applied to micro-structured media, was challenged by novel and unexpected experimental results. In particular, the synthesis of many complete series of fatty perindopril erbumine synthe
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For the derivatives a c another likely explanation for antif
2023-08-01

For the derivatives 3a–3c, another likely explanation for antifungal properties is that polymers bearing primary amine groups and secondary phosphoryl groups formed, enhancing complexation with the phosphate groups, and the complexes are amphiphilic (Palermo, Lee, Ramamoorthy, & Kuroda, 2011). The a
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